Evidence map›Paper›PMID 32280198›Full record

ArticleDrug design, development and therapy2020

Pre-Clinical Pharmacokinetics, Tissue Distribution and Physicochemical Studies of CLBQ14, a Novel Methionine Aminopeptidase Inhibitor for the Treatment of Infectious Diseases.

Oscar Ekpenyong, Xiuqing Gao, Jing Ma, Candace Cooper, Linh Nguyen, Omonike A Olaleye, Dong Liang, Huan Xie

Open access · goldAbstract read
In one paragraph

Article in Drug design, development and therapy, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
0.8field-weighted citation impact, top 27% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

7 citing papers in PubMed, 13 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. The Potential Role of the Methionine Aminopeptidase GeneInternational journal of molecular sciences · 2022
    Article
  5. Targeting Non-ReplicatingInternational journal of molecular sciences · 2021
    Review
  6. Article
  7. Potential therapeutic approaches for a sleeping pathogen: tuberculosis a case for bioinorganic chemistry.Journal of biological inorganic chemistry : JBIC : a publication of the Society of Biological Inorganic Chemistry · 2020
    Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors at 1 institution in 1 country.

Oscar EkpenyongDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.
Xiuqing GaoDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.
Jing MaDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.
Candace CooperDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.
Linh NguyenDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.
Omonike A OlaleyeDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.
Dong LiangDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.
Huan XieDepartment of Pharmaceutical and Environmental Health Sciences, College of Pharmacy and Health Sciences, Texas Southern University, Houston, TX, USA.ORCID 0000-0002-0591-5619
Texas Southern University · US

Funding

Targeted Nano-drug-delivery-systems of Frist-in-class Drugs for CRPC: PK/PD Evaluation and Combination TherapyU54MD007605 · NIMHD · TEXAS SOUTHERN UNIVERSITY · PI Song Gao · 2020 to 2026
$22.0M
Center for Biomedical and Health Research Excellence (CBHRE)G12MD007605 · NIMHD · TEXAS SOUTHERN UNIVERSITY · PI OYEKAN, ADEBAYO O., WILSON, BOBBY L · 2014 to 2018
$7.1M
Development of a Novel Nanoconstruct Based Photothermal Therapy for Tumor HypoxiaSC3GM102018 · NIGMS · TEXAS SOUTHERN UNIVERSITY · PI XIE, HUAN · 2012 to 2015
$449k
NIGMS NIH HHS SC3 GM102018NIMHD NIH HHS G12 MD007605NIMHD NIH HHS U54 MD007605
6 · The paper itself

Abstract

introductionCLBQ14, a derivative of 8-hydroxyquinoline, exerts its chemotherapeutic effect by inhibiting methionine aminopeptidase (MetAP), the enzyme responsible for the post-translational modification of several proteins and polypeptides. MetAP is a novel target for infectious diseases. CLBQ14 is selective and highly potent against replicating and latent

methodsThe physicochemical properties (solubility, pH stability and lipophilicity), in vitro plasma stability and metabolism, pre-clinical pharmacokinetics, plasma protein binding and tissue distribution of CLBQ14 in adult male Sprague-Dawley rats were characterized.

resultsAt room temperature, CLBQ14 is practically insoluble in water (<0.07 mg/mL) but freely soluble in dimethyl acetamide (>80 mg/mL); it has a log

conclusionCLBQ14 possess appealing qualities of a drug candidate. The studies reported herein are imperative to the development of CLBQ14 as a new chemical entity for infectious diseases.

Indexed as

AnimalsChemistry, PhysicalCommunicable DiseasesEnzyme InhibitorsHeartHumansKidneyMacaca fascicularisMaleMethionyl AminopeptidasesMiceMolecular StructureOxyquinolineRatsRats, Sprague-DawleyThermodynamicsEnzyme InhibitorsMethionyl AminopeptidasesOxyquinolinetilbroquinol8-hydroxyquinolineCLBQ14clioquinoldrug developmentmethionine aminopeptidasepharmacokineticsphysicochemicaltissue distribution

Identifiers

PMID32280198
PMCPMC7127848
OpenAlexW3013492986

What OpenQuestion holds

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LicenceCC BY-NC
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.